A8550-5mg | Telatinib (BAY 57-9352) [332012-40-5] Clinisciences

Background

Telatinib (BAY 57-9352) is a selective inhibitor of VEGFR2, VEGFR3, c-Kit and PDGFRα with IC50 value of 6 nM, 4 nM, 1 nM and 15 nM, respectively [1].

Vascular endothelial growth factor receptor (VEGFR) is the receptor of VEGF and plays an important role in stimulating vasculogenesis and angiogenesis. Platelet-derived growth factor (PDGF) is a member of growth factors and involves in blood vessel formation. C-Kit is the receptor of a growth factor. Many studies have shown that abnormal of VEGFR, c-Kit and PDGFR are correlated with a variety of tumors [1, 2, 3].

Telatinib is a potent VEGFR2/3, c-Kit and PDGFRα inhibitor. When tested with a panel of tumor cell lines (MDA-MB-231 breast caicinoma, Colo-205 colon carcinoma, DLD-1 colon carcinoma and H460 non-small cell lung carcinoma), Telatinib treatment exhibited inhibition on VEGFR-2 autophosphorylation and PDGF-βwhich involved in the angiogenic process [2].

Telatinib has been used in clinical trails to a variety of cancers treatment and has achieved promising results [2-4].

It is also reported that Telatinib restores tumor cells sensitivity to anticancer drugs and significantly reduced cellular viability by inhibiting ABCG2 expression [3].

References:
[1]. Steeghs, N., et al., Hypertension and rarefaction during treatment with telatinib, a small molecule angiogenesis inhibitor. Clin Cancer Res, 2008. 14(11): p. 3470-6.
[2]. Strumberg, D., et al., Phase I dose escalation study of telatinib (BAY 57-9352) in patients with advanced solid tumours. Br J Cancer, 2008. 99(10): p. 1579-85.
[3]. Sodani, K., et al., Telatinib reverses chemotherapeutic multidrug resistance mediated by ABCG2 efflux transporter in vitro and in vivo. Biochem Pharmacol, 2014. 89(1): p. 52-61.
[4]. Eskens, F.A., et al., Phase I dose escalation study of telatinib, a tyrosine kinase inhibitor of vascular endothelial growth factor receptor 2 and 3, platelet-derived growth factor receptor beta, and c-Kit, in patients with advanced or metastatic solid tumors. J Clin Oncol, 2009. 27(25): p. 4169-76.

Chemical Properties

Physical Appearance	A solid
Storage	Store at -20°C
M.Wt	409.83
Cas No.	332012-40-5
Formula	C₂₀H₁₆ClN₅O₃
Synonyms	BAY 579352;BAY 57 9352
Solubility	insoluble in H2O; insoluble in EtOH; ≥20.5 mg/mL in DMSO
Chemical Name	4-[[4-(4-chloroanilino)furo[2,3-d]pyridazin-7-yl]oxymethyl]-N-methylpyridine-2-carboxamide
SDF	Download SDF
Canonical SMILES	CNC(=O)C1=NC=CC(=C1)COC2=NN=C(C3=C2OC=C3)NC4=CC=C(C=C4)Cl
Shipping Condition	Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips	We do not recommend long-term storage for the solution, please use it up soon.

Biological Activity

Description	Telatinib is a potent inhibitor of VEGFR2/3, c-Kit and PDGFRβ with IC50 values of 6 nM/4 nM, 1 nM and 15 nM, respectively.
Targets	c-Kit	VEGFR3	VEGFR2	PDGFRα
IC50	1 nM	4 nM	6 nM	15 nM